Gynepristone

Gynepristone, also known as mifepristone, is a drug used for medical abortion. It is an antiprogestogen, meaning it blocks the action of progesterone, a hormone needed to maintain pregnancy.

Mifepristone is usually used in combination with prostaglandins (usually misoprostol), which helps to cause the uterus to contract and release the contents of the uterus, which results in termination of pregnancy.

This drug can be used in a medical setting under strict supervision and guidance of a physician. It is often offered as an alternative to surgical abortion, especially in early pregnancy. In some countries, mifepristone can also be prescribed for medical abortion at home, but this requires strict adherence to instructions and supervision by a physician.

It is important to note that the use of mifepristone can have side effects and risks, so its use should only be carried out under the supervision of a qualified healthcare professional.

Indications Gynepristone

1. Medical termination of pregnancy: Mifepristone can be used for medical termination of pregnancy during the first 7-9 weeks of pregnancy. It is used in combination with a prostaglandin (usually misoprostol) to induce an abortion.
2. Abortion for missed abortion or embryonic death: In some cases, the pregnancy may end on its own, but the fetal remains may still remain in the uterus. In such cases, mifepristone may be used to help remove the fetal remains.
3. Termination of dangerous pregnancy: In rare cases, pregnancy may pose a risk to the health of the mother. In such situations, mifepristone may be used to terminate the pregnancy.
4. Research studies: Mifepristone may also be used in research studies related to pregnancy termination or its consequences.

Release form

Gynepristone, also known as mifepristone, is usually available as a tablet to take orally. This drug is used medically to terminate early pregnancy.

Typically, the method of administration and dosage of Ginepristone (mifepristone) are determined by the doctor and may depend on the individual characteristics of the patient and the specific situation. However, in general, the use of the drug may look like this:

1. First Dose: Usually, the patient takes one tablet of Gynepristone (mifepristone) under the supervision of a doctor in a medical facility.
2. Second dose: Usually 24 to 48 hours after taking mifepristone, the patient takes a second dose of the drug - progesterone (usually misoprostol) - also under the doctor's supervision.

It is important to remember that the dosage and regimen should be determined only under the supervision of a qualified medical professional. Patients should strictly follow the doctor's instructions and not change the dosage or regimen without his or her consent.

Pharmacodynamics

1. Mechanism of action:

   • Ginepristone is an antiprogesterone. It binds to progesterone receptors, blocking their activity.
   • Progesterone is necessary to maintain pregnancy, so blocking its receptors leads to the destruction of the endometrium (the inner lining of the uterus), which leads to the rejection of the fetus or embryo.
   • Gynepristone also stimulates contraction of the uterine muscle, which helps to expel the contents of the uterus.

2. Use in medicine:

   • For medical abortion: Gynepristone is often used in combination with prostaglandins (such as misoprostol) to induce an abortion.
   • For the treatment of hyperprolactinemia: Gynepristone can be used to reduce prolactin levels in the blood by blocking prolactin receptors in the pituitary gland.

3. Efficiency and safety:

   • Gynepristone is generally considered effective and safe for medical abortion, especially in the early stages of pregnancy. However, it is important to use it under the supervision of a trained medical professional due to potential complications.
   • As with any medication, side effects such as bleeding, abdominal pain, nausea and vomiting may occur.

Pharmacokinetics

1. Absorption: Mifepristone is generally well absorbed from the gastrointestinal tract after oral administration. The time to reach peak blood concentrations is usually several hours.
2. Metabolism: Mifepristone is metabolized in the liver to form active and inactive metabolites. This occurs primarily through oxidation and hydroxylation processes.
3. Elimination: Mifepristone and its metabolites are usually excreted via bile and urine. The elimination half-life may be long due to the long half-life in blood.
4. Interactions with food and other drugs: Food may affect the rate and extent of absorption of mifepristone. Some drugs may affect its metabolism and elimination, which may require dosage adjustments or monitoring.
5. Kinetics in different populations: The kinetics of mifepristone may vary in different populations, including pregnant women, the elderly, and patients with hepatic or renal impairment. This may require individualization of dosage or monitoring for adverse effects.

Dosing and administration

Gynepristone, also known as mifepristone, is commonly used to terminate an early pregnancy. Here is the typical route of administration and dosage:

1. First Dose: Usually, the patient takes one tablet of Gynepristone (mifepristone) orally under the supervision of a physician in a medical facility. This usually occurs within the first few days after pregnancy is confirmed.

2. Second dose: After a certain period of time (usually 24-48 hours) after taking mifepristone, the patient takes a second dose of a progesterone medication, most often misoprostol, which helps complete the abortion process. This is also done under the supervision of a doctor.

The dosage and regimen may vary depending on the individual characteristics of the patient and the doctor's recommendations. It is important for patients to strictly follow the doctor's instructions and not change the dosage or regimen without his or her consent. Before starting treatment with Gynepristone (mifepristone), it is recommended to discuss possible risks and side effects with a healthcare professional.

Use Gynepristone during pregnancy

Mifepristone (also known as RU-486) is used for medical termination of early pregnancy. It is an antiprogesterone drug that blocks the action of progesterone, which is necessary to maintain pregnancy. In clinical studies, Mifepristone has been used in combination with misoprostol to terminate pregnancies up to 9 weeks with high efficacy and good tolerability.

Uses of Mifepristone include:

1. Induction of cervical ripening before early surgical abortion.
2. Termination of pregnancy in the first trimester by combination with prostaglandin for effective medical abortion.

Studies show that mifepristone is effective in terminating pregnancy up to 9 weeks. The success rate is about 92% at 49 days and decreases to 77% at 57 to 63 days (Spitz et al., 1998). It is important to note that the use of Mifepristone is not recommended if the pregnancy is desired and is planned to be continued, as this substance is intended to terminate it.

Contraindications

1. Confirmed or suspected pregnancy beyond the stated period: Mifepristone should not be used if pregnancy is confirmed or suspected beyond the period established for safe use of the drug.
2. Acute or chronic adrenal disease: Patients with acute or chronic adrenal disease may have an increased risk of complications when using mifepristone.
3. Use of corticosteroids: Mifepristone should not be used in patients taking high doses of corticosteroids as it may increase the risk of adverse effects.
4. Taking anticoagulants: Taking mifepristone may enhance the effect of anticoagulants, which increases the risk of bleeding.
5. Hypersensitivity to the drug: People with known hypersensitivity to mifepristone or any other components of the drug should avoid its use.
6. Presence of rare hereditary diseases such as porphyria: In these cases, the use of mifepristone may be contraindicated due to the potential for worsening symptoms of the disease.

Side effects Gynepristone

1. Bleeding and bleeding: Bleeding may occur after using mifepristone and prostaglandins, and may be heavy or profuse.
2. Lower abdominal pain: Some women may experience lower abdominal pain or cramping, which may be accompanied by contractions.
3. Headache and Dizziness: Some patients may experience headache or dizziness during or after the procedure.
4. Nausea and vomiting: These symptoms may also occur as a result of using mifepristone and prostaglandins.
5. Fatigue and weakness: Some women may feel tired or weak after the procedure.
6. Emotional changes: Some patients may experience emotional changes such as anxiety, sadness, or irritability.

Overdose

Overdose of gynepristone (mifepristone) can have serious consequences and require immediate medical attention. Since gynepristone is used for medical purposes, its dosage and use should be strictly controlled by a doctor.

Overdose symptoms can vary and may include uterine bleeding, abdominal pain, nausea, vomiting, dizziness, fainting, and other unpleasant conditions.

Interactions with other drugs

1. Drugs that affect cytochrome P450: Mifepristone is metabolized in the liver via cytochrome P450 enzymes. Drugs that are inhibitors or inducers of these enzymes may affect the metabolism of mifepristone and alter its blood concentrations. For example, cytochrome P450 inhibitors such as ketoconazole or rifampicin may increase or decrease mifepristone blood concentrations, which may require dosage adjustments.
2. Antihistamines: Mifepristone may enhance the sedative effects of antihistamines, which may result in increased drowsiness.
3. Hormonal drugs: Mifepristone affects the hormonal balance in the body, so using it with other hormonal drugs, such as contraceptives or hormone replacement therapy, may lead to changes in the effectiveness of their action.
4. Anticoagulants: Mifepristone may affect the metabolism of vitamin K, which may increase or decrease the effect of anticoagulants. Patients taking anticoagulants should consult a physician for dosage adjustments and monitoring.
5. Anticancer drugs: Interactions between mifepristone and anticancer drugs may alter their effectiveness or toxicity. Cancer patients should inform their physician of all medications they are taking.

Storage conditions

1. Temperature: It is generally recommended to store Gynepristone at room temperature, between 20°C and 25°C. Sometimes a slight deviation from these limits is allowed, but it is important to avoid extreme temperatures.
2. Humidity: The product should be stored in a dry place, protected from humidity. High humidity may affect the stability of the product.
3. Light: Store Gynepristone in a dark place away from direct sunlight. Light can degrade the active ingredients of the drug.
4. Packaging: Follow the instructions on the package to ensure proper storage of the product.